|Single-dose pharmacokinetics and safety of iptakalim hydrochloride in Chinese healthy volunteers|
|Cai, Yun1; Chai, Dong1; Pei, Fei1; Fang, Yi3; Wang, Rui1; Liang, Bei-bei1; Cui, Wen-yu2,4; Bao, Cun-gang4; Wang, Hai2,4,5|
|关键词||Food Effect Iptakalim Pharmacokinetics Phase i Safety|
|刊名||JOURNAL OF PHARMACY AND PHARMACOLOGY|
|WOS标题词||Science & Technology|
|类目[WOS]||Pharmacology & Pharmacy|
|研究领域[WOS]||Pharmacology & Pharmacy|
|关键词[WOS]||PROTECTING ENDOTHELIAL FUNCTION ; POTASSIUM CHANNEL OPENERS ; ATP ; HYPERTENSION ; CELLS ; ACTIVATION ; PRESSURE|
Objectives To investigate the safety, pharmacokinetics and food effect of iptakalim in healthy adult Han Chinese volunteers.
Methods Study 1 was a randomized open-label, Latin square designed, single-dose, three-period, self-control crossover study. Six men and six women received 5, 10 and 20 mg of iptakalim orally. Study 2 was a randomized, open-label, single-dose, two-period, self-control crossover study. Ten men were included and each subject received 5 mg iptakalim orally, fasting and nonfasting. Key findings No adverse effects were reported and no clinically meaningful changes in vital signs were found. Cmax, AUC(0-t) and AUC(0-infinity) were proportional over the dose levels of 5, 10 and 20 mg. Tmax, t1/2 and CL/F were similarly independent of dose level. In the 5 mg and 20 mg group, the Cmax, AUC0-t and AUC(0-infinity) in women were significantly higher than in men, although they showed no difference after correction by mg/kg doses in the 5 mg group. At the 5-mg dose level, no significant difference in pharmacokinetics was found in nonfasting and fasting subjects.
Conclusions Single-dose pharmacokinetics of iptakalim showed dose proportionality over the dose levels of 5-20 mg. The pharmacokinetics showed gender differences in the 5 and 20 mg groups. Food had almost no impact on the pharmacokinetics at the 5 mg level.
|项目编号||2008ZX09101-006 ; D0204003040721 ; 02C26213200052|
|资助机构||major national science and technology special projects for new drug ; major projects of Beijing science and technology ; national technical innovation projects|
|作者单位||1.Thadweik Acad Med, Beijing, Peoples R China|
2.Tianjin Inst Hyg & Environm Med, Tianjin, Peoples R China
3.Peoples Liberat Army Gen Hosp, Dept Clin Pharmacol, Beijing 100853, Peoples R China
4.Peking Univ, Peoples Hosp, Dept Cardiovasc Pharmacol, Inst Pharmacol & Toxicol, Beijing 100871, Peoples R China
5.Peking Univ, Peoples Hosp, Dept Pharm, Beijing 100871, Peoples R China
|Cai, Yun,Chai, Dong,Pei, Fei,et al. Single-dose pharmacokinetics and safety of iptakalim hydrochloride in Chinese healthy volunteers[J]. JOURNAL OF PHARMACY AND PHARMACOLOGY,2012,64(3):337-343.|
|APA||Cai, Yun.,Chai, Dong.,Pei, Fei.,Fang, Yi.,Wang, Rui.,...&Wang, Hai.(2012).Single-dose pharmacokinetics and safety of iptakalim hydrochloride in Chinese healthy volunteers.JOURNAL OF PHARMACY AND PHARMACOLOGY,64(3),337-343.|
|MLA||Cai, Yun,et al."Single-dose pharmacokinetics and safety of iptakalim hydrochloride in Chinese healthy volunteers".JOURNAL OF PHARMACY AND PHARMACOLOGY 64.3(2012):337-343.|